Biotransformation reactions can lead to any one of the following:
  • Inactivation – most drugs are rendered pharmacologically inactive
    • Example: Many drugs - morphine, chloramphenicol, procaine etc.
  • Formation of active metabolite – the metabolite formed possesses biological activity
    • Ciprofloxacin from enrofloxacin
    • Oxyphenbutazone from Phenylbutazone
    • Salicylic acid from aspirin
  • Inactive drug to active drug (Prodrug) An inactive drug gets converted into an active metabolite once it undergoes biotransfomation inside the body
    • Example:
      • Hetacillin to ampicillin 
      • Prontosil to sulfanilamide
  • Less active or inactive drug is converted into a more toxic drug (Lethal synthesis)
    • Example:
      • Parathion to paraoxon
      • Fluoroacetic acid to fluorocitrate

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